Targeted antifungal delivery system: b-Glucosidase sensitive nystatin-star poly(ethylene glycol) conjugate

A new targeted intravenous conjugate of nystatin with pentaerythritol poly(ethylene glycol)ether has been prepared and characterised (NY sub(4)-sPEG, M = 25 160). The conjugate contains a b-d-glucopyranoside molecular switch sensitive to b-glucosidases (E.C.3.2.1.21), which are specifically present...

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Bibliographic Details
Published in:International journal of pharmaceutics 2010-02, Vol.386 (1-2), p.1-5
Main Authors: Bilkova, Eliska, Imramovsky, Ales, Buchta, Vladimir, Sedlak, Milos
Format: Article
Language:English
Subjects:
Aspergillus niger
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Summary:A new targeted intravenous conjugate of nystatin with pentaerythritol poly(ethylene glycol)ether has been prepared and characterised (NY sub(4)-sPEG, M = 25 160). The conjugate contains a b-d-glucopyranoside molecular switch sensitive to b-glucosidases (E.C.3.2.1.21), which are specifically present in the enzyme outfit of fungal pathogens. The investigated conjugate is stable under in vitro conditions for 24 h (solution of phosphate buffer pH = 7.4). Spectrophotometrically controlled releasing of nystatin in model medium containing b-glucosidase ((Aspergillus niger) 2 mg/mL, 66.6 units/g; pH 7.4, 2 x 10 super(-2) M), reported decomposition half-life of conjugate t sub(1/2) = (88 +/- 2) s. This implies that releasing of nystatin is controlled only enzymatically.
ISSN:0378-5173
DOI:10.1016/j.ijpharm.2009.10.034